2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PCSK9-IN-10

PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.

For research use only. We do not sell to patients.

PCSK9-IN-10 Chemical Structure

PCSK9-IN-10 Chemical Structure

CAS No. : 368434-98-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PCSK9-IN-10 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].

In Vitro

PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) significantly decreases the PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PCSK9-IN-10 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cells
Concentration: 0-1000 µM
Incubation Time: 24 h
Result: Showed low cytotoxicity to HepG2 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0, 2.5, 5, 12.5, 25 µM
Incubation Time: 24 h
Result: Significantly decreased PCSK9 protein level in a dose dependent manner.
In Vivo

PCSK9-IN-10 (30 mg/kg; p.o.; once a day for 8 weeks) reduces total cholesterol (TC) and atherosclerotic plaque size in ApoE KO mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight weeks old male ApoE KO mice[1]
Dosage: 30 mg/kg
Administration: P.o.; once a day for 8 weeks
Result: Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size.
Molecular Weight

373.41

Formula

C18H23N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)N(C)C2=C(N(CC3=CC=CC(OC)=C3)C(NCCOC)=N2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (669.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6780 mL 13.3901 mL 26.7802 mL
5 mM 0.5356 mL 2.6780 mL 5.3560 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6780 mL 13.3901 mL 26.7802 mL 66.9505 mL
5 mM 0.5356 mL 2.6780 mL 5.3560 mL 13.3901 mL
10 mM 0.2678 mL 1.3390 mL 2.6780 mL 6.6951 mL
15 mM 0.1785 mL 0.8927 mL 1.7853 mL 4.4634 mL
20 mM 0.1339 mL 0.6695 mL 1.3390 mL 3.3475 mL
25 mM 0.1071 mL 0.5356 mL 1.0712 mL 2.6780 mL
30 mM 0.0893 mL 0.4463 mL 0.8927 mL 2.2317 mL
40 mM 0.0670 mL 0.3348 mL 0.6695 mL 1.6738 mL
50 mM 0.0536 mL 0.2678 mL 0.5356 mL 1.3390 mL
60 mM 0.0446 mL 0.2232 mL 0.4463 mL 1.1158 mL
80 mM 0.0335 mL 0.1674 mL 0.3348 mL 0.8369 mL
100 mM 0.0268 mL 0.1339 mL 0.2678 mL 0.6695 mL
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PCSK9-IN-10 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCSK9-IN-10368434-98-4PCSK9Proprotein convertase subtilisin/kexin type 9HepG2 cellsLDLRtotal cholesterolatherosclerotic plaquehyperlipidemiaInhibitorinhibitorinhibit

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